CAS: 19563-04-3; 4-Chlorobenzenecarboximidamide

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CAS号40546-41-6 4-氯苯亚胺酸乙酯 | CAS号623-03-0 对氯苯腈 | CAS号631-61-8 乙酸铵 | CAS号98-10-2 苯磺酰胺 | CAS号74-11-3 对氯苯甲酸 | CAS号304693-56-9 4-氯-2-(4-氯苯基)嘧啶... | CAS号100558-20-1 2-(4-chlorophen...

📜对氯苯甲腈置于sodium Methylate,氯化铵体系中,用 甲醇 用作溶剂,化学反应 48.0H,反应生成对氯苯甲脒
参考文献:抗恶性黑色素瘤的新型脱氧马尿苷合酶变构抑制剂:设计,合成和生物学评价
标题:抗恶性黑色素瘤的新型脱氧马尿苷合酶变构抑制剂:设计,合成和生物学评价
摘要:基于脱氧马尿苷合酶(Dhps)的新型变构位点,设计并合成了两个系列的30种新型5-(2-甲氧基苯氧基)-2-苯基嘧啶-4-胺衍生物作为dhps抑制剂.其中,化合物8M的dhps抑制效力最好(ic 50 = 0.014 μm),对黑色素瘤细胞表现出优异的抑制作用,优于gc7.此外,分子对接和分子动力学(md)模拟进一步证明化合物8M与dhps的变构位点紧密结合.流式细胞术分析和酶联免疫吸附测定(elisa)表明化合物8M可以抑制细胞内活性氧(ros)水平.此外,通过蛋白质印迹分析,化合物8M有效激活caspase 3并降低gp-100,酪氨酸酶,Eif5A2,Mmp2和mmp9的表达.此外,Transwell分析和伤口愈合分析均表明化合物8M可以抑制黑色素瘤细胞的侵袭和迁移.在体内研究中,肿瘤异种移植模型表明,化合物8M能有效抑制黑色素瘤的发展,且毒性低.
Doi:10.1021/acs.Jmedchem.1C00582

专利信息

专利号:US-7501407-B2
优先权日:2001-12-20
标题 :Pyrimidine A2B selective antagonist compounds, their synthesis and use
发明人：CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO; COLLINGTON ERIC
权利人:OSI PHARM INC
摘要:The subject invention provides compounds having the structure: n nwherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R 2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R 3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 2 and R 3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R 3 is oxygen; R 4 and R 5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 4 NR 5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms;n R 12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A 2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

专利号:CN-118086928-A
优先权日:2022-11-25
标 题:Method for electrochemical synthesis of pyrimidoindole derivative under mild condition

专利号:MX-PA04005862-A
优先权日:2001-12-20
标 题 :SELECTED ANTAGONIST COMPOUNDS OF PYRIMIDINE A2B, ITS SYNTHESIS AND USE.